Tranzyme Pharma Inc., a leading biopharmaceutical company developing small molecule therapeutics for the treatment of gastrointestinal (GI) disorders, has announced efficacy data for TZP-101, the company’s lead product for the treatment of postoperative ileus and diabetic gastroparesis.

TZP-101 is a small molecule ghrelin receptor agonist, which has been shown to selective stimulate motility of the GI tract. In a presentation at the 20th International Symposium on Neurogastroenterology & Motility (Toulouse, France), Tranzyme Pharma presented new in vivo data demonstrating that the potent and selective gastroprokinetic activity of TZP-101 takes place without the release of growth hormone.

Ghrelin is a peptide hormone known to stimulate both gastrointestinal motility and growth hormone release. Tranzyme Pharma has applied its proprietary chemistry technology to dissociate these two aspects of ghrelin pharmacology resulting in a product profile with selectivity for the treatment of gastrointestinal disorders.

“Our discovery that TZP-101 effectively separates the gastroprokinetic and endocrine effects of ghrelin is a significant breakthrough in ghrelin receptor pharmacology,” said Dr Graeme L Fraser, vice president of Drug Discovery.

“By eliminating the growth hormone secretagogue aspects of ghrelin receptor stimulation, we expect that TZP-101 will avoid significant potential side-effects when it is used for chronic therapeutic indications such as gastroparesis,” Fraser added.

“These data further validate the ability of Tranzyme Pharma’s small molecule chemistry to design compounds with great selectivity towards multimeric targets such as GPCRs, kinases and ion channels,” said Lindsay N Donald, DABT, vice president of Business and Preclinical Development.

“Traditionally, this sort of selectivity has only been possible with peptide or protein therapeutics. Our chemistry technology allows us to maintain the favorable binding characteristics of large biomolecules while eliminating their drawbacks such as low oral bioavailability, high manufacturing costs, and antigenicity,” Donald added.